Gossypol, a polyphenolic aldehyde extracted from cottonseed, is a male anti-fertility agent which has been reported to have anti-viral activity. In this paper we report that gossypol inactivates human immunodeficiency virus (HIV) in an in vitro system. Following exposure of cell-free incubates of HIV to 100 uM gossypol, ultracentrifugation and inoculation of the washed pellet onto H9 cells, there is no evidence of elevated reverse transcriptase activity over 21 days. Treatment with lower concentrations of gossypol reduces the peak and lengthens the time to maximal reverse transcriptase activity compared with control cultures. These observations suggest that gossypol could be used as a vaginal spermicidal/virucidal agent. The mechanism of the in vitro anti-viral action as well as the effect of orally administered gossypol on the infectivity of semen of HIV-seropositive men warrant further study.
PIP: Following research that demonstrated the quality of gossypol, a polyphenolic aldehyde taken from cottonseed, in causing anti-viral activity, testing was done in pursuit of the inactivation of Human Immunodeficiency Virus in vitro. Gossypol is an orally active male anti-fertility agent that has been used in China by more than 10,000 men. Its biological abilities and effects include both anti-viral and anti-parasitic activity. virucidal activity has been observed against many diseases including herpes simplex-2. Thus, the preventative applications for gossypol are evident particularly as a spermicidal/virucidal agent used as a vaginal contraceptive. Gossypol can be absorbed by women vaginally. In the testing of the possibility of the inactivation of HIV, it was found that a concentration of 100uM of gossypol completely inactivates cell-free preparations of HIV. Although the applications for the use of gossypol as a vaginal preparation are apparent, further research and testing is needed of a process that limits or reduces the virus content, especially among seropositive men, and a process that affects the infectivity of semen at the point of ejaculation.